SG195172A1 - Novel maytansinoid derivatives with peptide linker and conjugates thereof - Google Patents

Novel maytansinoid derivatives with peptide linker and conjugates thereof

Info

Publication number
SG195172A1
SG195172A1 SG2013087556A SG2013087556A SG195172A1 SG 195172 A1 SG195172 A1 SG 195172A1 SG 2013087556 A SG2013087556 A SG 2013087556A SG 2013087556 A SG2013087556 A SG 2013087556A SG 195172 A1 SG195172 A1 SG 195172A1
Authority
SG
Singapore
Prior art keywords
conjugates
formula
peptide linker
novel
maytansinoid derivatives
Prior art date
Application number
SG2013087556A
Other languages
English (en)
Inventor
Wayne C Widdison
Original Assignee
Immunogen Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Immunogen Inc filed Critical Immunogen Inc
Publication of SG195172A1 publication Critical patent/SG195172A1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C07D207/416—2,5-Pyrrolidine-diones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/0005—Vertebrate antigens
    • A61K39/0011—Cancer antigens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6849—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A61K47/6863—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from stomach or intestines cancer cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/21—Immunoglobulins specific features characterized by taxonomic origin from primates, e.g. man

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Cell Biology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Mycology (AREA)
  • Communicable Diseases (AREA)
  • Microbiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
SG2013087556A 2011-06-21 2012-06-21 Novel maytansinoid derivatives with peptide linker and conjugates thereof SG195172A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161499548P 2011-06-21 2011-06-21
PCT/US2012/043488 WO2012177837A2 (en) 2011-06-21 2012-06-21 Novel maytansinoid derivatives with peptide linker and conjugates thereof

Publications (1)

Publication Number Publication Date
SG195172A1 true SG195172A1 (en) 2013-12-30

Family

ID=46889411

Family Applications (2)

Application Number Title Priority Date Filing Date
SG2013087556A SG195172A1 (en) 2011-06-21 2012-06-21 Novel maytansinoid derivatives with peptide linker and conjugates thereof
SG10201605041VA SG10201605041VA (en) 2011-06-21 2012-06-21 Novel maytansinoid derivatives with peptide linker and conjugates thereof

Family Applications After (1)

Application Number Title Priority Date Filing Date
SG10201605041VA SG10201605041VA (en) 2011-06-21 2012-06-21 Novel maytansinoid derivatives with peptide linker and conjugates thereof

Country Status (14)

Country Link
US (2) US9289512B2 (es)
EP (1) EP2723389A2 (es)
JP (2) JP6209159B2 (es)
KR (1) KR20140037208A (es)
CN (1) CN103648532A (es)
AU (1) AU2012272930B2 (es)
BR (1) BR112013032928A2 (es)
CA (1) CA2836927A1 (es)
EA (2) EA029797B1 (es)
IL (2) IL230043A (es)
MX (1) MX350954B (es)
SG (2) SG195172A1 (es)
WO (1) WO2012177837A2 (es)
ZA (1) ZA201308703B (es)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1789391B1 (en) 2004-07-23 2017-06-28 Endocyte, Inc. Bivalent linkers and conjugates thereof
AU2008224988A1 (en) 2007-03-14 2008-09-18 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
US9138484B2 (en) 2007-06-25 2015-09-22 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
EA029797B1 (ru) 2011-06-21 2018-05-31 Иммуноджен, Инк. Новые производные майтанзиноида с пептидным линкером и их конъюгаты
WO2013126797A1 (en) 2012-02-24 2013-08-29 Purdue Research Foundation Cholecystokinin b receptor targeting for imaging and therapy
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
JP6239597B2 (ja) 2012-05-15 2017-11-29 ソレント・セラピューティクス・インコーポレイテッドＳｏｒｒｅｎｔｏ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． 薬物コンジュゲート、コンジュゲーション方法およびその使用
SG11201502896XA (en) 2012-10-16 2015-05-28 Endocyte Inc Drug delivery conjugates containing unnatural amino acids and methods for using
US9353150B2 (en) 2012-12-04 2016-05-31 Massachusetts Institute Of Technology Substituted pyrazino[1′,2′:1 ,5]pyrrolo[2,3-b]-indole-1,4-diones for cancer treatment
MY169117A (en) 2012-12-21 2019-02-18 Bioalliance Cv Hydrophilic self-immolative linkers and conjugates thereof
KR102306490B1 (ko) * 2013-03-15 2021-09-28 리제너론 파아마슈티컬스, 인크. 생물학적 활성 분자, 그의 접합체 및 치료 용도
US10208125B2 (en) 2013-07-15 2019-02-19 University of Pittsburgh—of the Commonwealth System of Higher Education Anti-mucin 1 binding agents and uses thereof
KR102252925B1 (ko) 2013-08-26 2021-05-18 리제너론 파마슈티칼스 인코포레이티드 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도
WO2015057876A1 (en) 2013-10-15 2015-04-23 Sorrento Therapeutics Inc. Drug-conjugates with a targeting molecule and two different drugs
WO2015196167A1 (en) 2014-06-20 2015-12-23 Bioalliance C.V. Anti-folate receptor aplha (fra) antibody-drug conjugates and methods of using thereof
CN110478495A (zh) 2014-06-30 2019-11-22 塔弗达治疗有限公司 靶向缀合物及其颗粒和制剂
CA2958882A1 (en) 2014-09-02 2016-03-10 Immunogen, Inc. Methods for formulating antibody drug conjugate compositions
SG11201701384XA (en) 2014-10-14 2017-03-30 Polytherics Ltd Process for the conjugation of a peptide or protein with a reagent comprising a leaving group including a portion of peg
CA2975383C (en) 2015-01-28 2023-09-12 Sorrento Therapeutics, Inc. Antibody drug conjugates comprising dolastatin derivatives
CN107995912A (zh) * 2015-03-27 2018-05-04 里珍纳龙药品有限公司 美登素类衍生物、其偶联物和使用方法
CN106380508A (zh) * 2015-07-28 2017-02-08 上海皓元生物医药科技有限公司 一种抗体偶联药物连接子的工业化生产方法
CN108473538B (zh) 2015-10-28 2022-01-28 塔弗达治疗有限公司 Sstr靶向缀合物及其颗粒和制剂
TWI753875B (zh) 2016-01-08 2022-02-01 美商美國全心醫藥生技股份有限公司 四價抗psgl-1抗體及其用途
SG11201806322QA (en) * 2016-01-25 2018-08-30 Regeneron Pharma Maytansinoid derivatives, conjugates thereof, and methods of use
RU2018130108A (ru) * 2016-02-05 2020-03-06 Иммуноджен, Инк. Эффективный способ получения конъюгатов связывающийся с клеткой агент цитотоксический агент
WO2017197045A1 (en) 2016-05-11 2017-11-16 Movassaghi Mohammad Convergent and enantioselective total synthesis of communesin analogs
CA3037732A1 (en) 2016-09-23 2018-03-29 Regeneron Pharmaceuticals, Inc. Anti-steap2 antibodies, antibody-drug conjugates, and bispecific antigen-binding molecules that bind steap2 and cd3, and uses thereof
US20180140703A1 (en) * 2016-11-18 2018-05-24 The Regents Of The University California Tumor radiosensitization with antibody conjugates
RU2765098C2 (ru) * 2017-02-28 2022-01-25 Иммуноджен, Инк. Производные майтанзиноида с саморасщепляющимися пептидными линкерами и их конъюгаты
WO2018209239A1 (en) 2017-05-11 2018-11-15 Massachusetts Institute Of Technology Potent agelastatin derivatives as modulators for cancer invasion and metastasis
EP3769786A4 (en) * 2017-06-19 2021-12-08 Sichuan Baili Pharm Co. Ltd ANTIBODY-DRUG CONJUGATE WITH AN ACID SELF-STABILIZATION JUNCTION
US10640508B2 (en) 2017-10-13 2020-05-05 Massachusetts Institute Of Technology Diazene directed modular synthesis of compounds with quaternary carbon centers
SG11202106593UA (en) 2018-12-21 2021-07-29 Avidity Biosciences Inc Anti-transferrin receptor antibodies and uses thereof
AU2020214796A1 (en) 2019-01-30 2021-07-29 Truebinding, Inc. Anti-Gal3 antibodies and uses thereof
CN109939242B (zh) * 2019-03-18 2020-10-09 北京大学 抗体前药偶联物及其制备和应用
US11535634B2 (en) 2019-06-05 2022-12-27 Massachusetts Institute Of Technology Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
CN110501495A (zh) * 2019-08-27 2019-11-26 广东菲鹏生物有限公司 活化氨基固相颗粒与免疫氨基固相颗粒及其制备方法和应用及试剂盒
JP2023537798A (ja) 2020-03-19 2023-09-06 アビディティー バイオサイエンシーズ，インク． 顔面肩甲上腕型筋ジストロフィーを処置するための組成物および方法
US11446387B2 (en) 2020-03-27 2022-09-20 Avidity Biosciences, Inc. Compositions and methods of treating muscle dystrophy
US12030888B2 (en) 2021-02-24 2024-07-09 Massachusetts Institute Of Technology Himastatin derivatives, and processes of preparation thereof, and uses thereof
US12036286B2 (en) 2021-03-18 2024-07-16 Seagen Inc. Selective drug release from internalized conjugates of biologically active compounds
EP4370555A1 (en) 2021-07-13 2024-05-22 TrueBinding, Inc. Methods of preventing protein aggregation
KR20240055874A (ko) 2021-09-16 2024-04-29 어비디티 바이오사이언시스 인크. 안면견갑상완 근이영양증을 치료하는 조성물 및 방법

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4307016A (en) 1978-03-24 1981-12-22 Takeda Chemical Industries, Ltd. Demethyl maytansinoids
US4256746A (en) 1978-11-14 1981-03-17 Takeda Chemical Industries Dechloromaytansinoids, their pharmaceutical compositions and method of use
JPS55102583A (en) 1979-01-31 1980-08-05 Takeda Chem Ind Ltd 20-acyloxy-20-demethylmaytansinoid compound
JPS55162791A (en) 1979-06-05 1980-12-18 Takeda Chem Ind Ltd Antibiotic c-15003pnd and its preparation
JPS5645483A (en) 1979-09-19 1981-04-25 Takeda Chem Ind Ltd C-15003phm and its preparation
EP0028683A1 (en) 1979-09-21 1981-05-20 Takeda Chemical Industries, Ltd. Antibiotic C-15003 PHO and production thereof
JPS5645485A (en) 1979-09-21 1981-04-25 Takeda Chem Ind Ltd Production of c-15003pnd
WO1982001188A1 (en) 1980-10-08 1982-04-15 Takeda Chemical Industries Ltd 4,5-deoxymaytansinoide compounds and process for preparing same
US4450254A (en) 1980-11-03 1984-05-22 Standard Oil Company Impact improvement of high nitrile resins
US4315929A (en) 1981-01-27 1982-02-16 The United States Of America As Represented By The Secretary Of Agriculture Method of controlling the European corn borer with trewiasine
US4313946A (en) 1981-01-27 1982-02-02 The United States Of America As Represented By The Secretary Of Agriculture Chemotherapeutically active maytansinoids from Trewia nudiflora
JPS57192389A (en) 1981-05-20 1982-11-26 Takeda Chem Ind Ltd Novel maytansinoid
US4894348A (en) * 1987-07-01 1990-01-16 Ronald Robert C Fluorescein-conjugated proteins with enhanced fluorescence
GB8801646D0 (en) * 1988-01-26 1988-02-24 Nycomed As Chemical compounds
US5171666A (en) * 1988-04-22 1992-12-15 Eli Lilly And Company Monoclonal antibodies reactive with a cell-surface gylcoprotein expressed on human carcinomas
CA2026147C (en) * 1989-10-25 2006-02-07 Ravi J. Chari Cytotoxic agents comprising maytansinoids and their therapeutic use
US5208020A (en) * 1989-10-25 1993-05-04 Immunogen Inc. Cytotoxic agents comprising maytansinoids and their therapeutic use
GB9015198D0 (en) 1990-07-10 1990-08-29 Brien Caroline J O Binding substance
ES2313867T3 (es) 1991-12-02 2009-03-16 Medical Research Council Produccion de anticuerpos anti-auto de repertorios de segmentos de anticuerpo expresados en la superficie de fagos.
ES2149768T3 (es) 1992-03-25 2000-11-16 Immunogen Inc Conjugados de agentes enlazantes de celulas derivados de cc-1065.
US5639641A (en) 1992-09-09 1997-06-17 Immunogen Inc. Resurfacing of rodent antibodies
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
US6355780B1 (en) 1995-02-22 2002-03-12 Yeda Research And Development Co. Ltd. Antibodies to the death domain motifs of regulatory proteins
WO1999006587A2 (en) 1997-08-01 1999-02-11 Morphosys Ag Novel method and phage for the identification of nucleic acid sequences encoding members of a multimeric (poly)peptide complex
US7115396B2 (en) 1998-12-10 2006-10-03 Compound Therapeutics, Inc. Protein scaffolds for antibody mimics and other binding proteins
CA2385528C (en) * 1999-10-01 2013-12-10 Immunogen, Inc. Compositions and methods for treating cancer using immunoconjugates and chemotherapeutic agents
WO2001038318A1 (en) 1999-11-24 2001-05-31 Immunogen, Inc. Cytotoxic agents comprising taxanes and their therapeutic use
US7097840B2 (en) * 2000-03-16 2006-08-29 Genentech, Inc. Methods of treatment using anti-ErbB antibody-maytansinoid conjugates
US6333410B1 (en) 2000-08-18 2001-12-25 Immunogen, Inc. Process for the preparation and purification of thiol-containing maytansinoids
WO2002020565A2 (en) 2000-09-08 2002-03-14 Universität Zürich Collections of repeat proteins comprising repeat modules
WO2002042259A2 (en) * 2000-11-27 2002-05-30 University Of Maryland, Baltimore Methods of synthesizing and using derivatives of [2-(2-aminoethoxy)ethoxy] acetic acid
US6441163B1 (en) 2001-05-31 2002-08-27 Immunogen, Inc. Methods for preparation of cytotoxic conjugates of maytansinoids and cell binding agents
AU2002363939A1 (en) * 2001-11-20 2003-06-10 Seattle Genetics, Inc. Treatment of immunological disorders using anti-cd30 antibodies
US6716821B2 (en) 2001-12-21 2004-04-06 Immunogen Inc. Cytotoxic agents bearing a reactive polyethylene glycol moiety, cytotoxic conjugates comprising polyethylene glycol linking groups, and methods of making and using the same
WO2003062198A1 (en) * 2002-01-24 2003-07-31 Barnes Jewish Hospital Integrin targeted imaging agents
US6756397B2 (en) 2002-04-05 2004-06-29 Immunogen, Inc. Prodrugs of CC-1065 analogs
US7659241B2 (en) 2002-07-31 2010-02-09 Seattle Genetics, Inc. Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease
EP1534674A4 (en) 2002-08-02 2007-11-28 Immunogen Inc CYTOTOXIC AGENTS CONTAINING NEW, EFFECTIVE TAXANES AND THEIR THERAPEUTIC USE
AU2003259163B2 (en) 2002-08-16 2008-07-03 Immunogen, Inc. Cross-linkers with high reactivity and solubility and their use in the preparation of conjugates for targeted delivery of small molecule drugs
WO2004043344A2 (en) 2002-11-07 2004-05-27 Immunogen, Inc. Anti-cd33 antibodies and method for treatment of acute myeloid leukemia using the same
US8088387B2 (en) 2003-10-10 2012-01-03 Immunogen Inc. Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates, and methods of making said conjugates
US7276497B2 (en) 2003-05-20 2007-10-02 Immunogen Inc. Cytotoxic agents comprising new maytansinoids
BR122018071808B8 (pt) * 2003-11-06 2020-06-30 Seattle Genetics Inc conjugado
JP4861308B2 (ja) 2004-04-07 2012-01-25 ジェネンテック， インコーポレイテッド 抗体結合体の質量分析
EP2286844A3 (en) 2004-06-01 2012-08-22 Genentech, Inc. Antibody-drug conjugates and methods
NZ553500A (en) 2004-09-23 2009-11-27 Genentech Inc Genentech Inc Cysteine engineered antibodies and conjugates withCysteine engineered antibodies and conjugates with a free cysteine amino acid in the heavy chain a free cysteine amino acid in the heavy chain
AU2005316844A1 (en) 2004-11-29 2006-06-22 Seattle Genetics, Inc. Engineered antibodies and immunoconjugates
US7301019B2 (en) 2005-01-21 2007-11-27 Immunogen, Inc. Method for the preparation of maytansinoid esters
US20060182750A1 (en) 2005-02-11 2006-08-17 Immunogen, Inc. Process for preparing stable drug conjugates
EA200702239A1 (ru) * 2005-04-15 2008-10-30 Иммьюноджен, Инк. Уничтожение гетерогенной или смешанной клеточной популяции в опухолях
US8846577B2 (en) 2005-07-08 2014-09-30 University Of Zurich Phage display using cotranslational translocation of fusion polypeptides
WO2007021674A2 (en) 2005-08-09 2007-02-22 Millennium Pharmaceuticals, Inc. Method of acylating maytansinol with chiral amino acids
EP1928503B1 (en) 2005-08-24 2012-10-03 ImmunoGen, Inc. Process for preparing maytansinoid antibody conjugates
JP5102772B2 (ja) 2005-11-29 2012-12-19 ザ・ユニバーシティ・オブ・シドニー デミボディ：二量体化活性化治療剤
US7897568B2 (en) 2006-03-03 2011-03-01 Vinay K. Singh Compositions for treatment of cancer
CA2655379A1 (en) 2006-06-22 2007-12-27 Walter And Eliza Hall Institute Of Medical Research Structure of the insulin receptor ectodomain
PE20090481A1 (es) 2007-07-16 2009-05-18 Genentech Inc Anticuerpos anti-cd79b e inmunoconjugados humanizados y metodos de uso
WO2009040338A1 (en) 2007-09-24 2009-04-02 University Of Zürich Designed armadillo repeat proteins
LT2281006T (lt) * 2008-04-30 2017-11-27 Immunogen, Inc. Skersinių jungčių linkeriai ir jų panaudojimas
WO2010093627A2 (en) 2009-02-12 2010-08-19 Centocor Ortho Biotech Inc. Fibronectin type iii domain based scaffold compositions, methods and uses
PL2437790T3 (pl) 2009-06-03 2019-09-30 Immunogen, Inc. Sposoby sprzęgania
WO2011100403A1 (en) 2010-02-10 2011-08-18 Immunogen, Inc Cd20 antibodies and uses thereof
UA123257C2 (uk) 2010-02-24 2021-03-10 Іммуноджен, Інк. Виділений поліпептид, що кодує антитіло до рецептора фолієвої кислоти 1
AU2011277999A1 (en) * 2010-07-12 2013-01-10 Covx Technologies Ireland Limited Multifunctional Antibody Conjugates
EA029797B1 (ru) 2011-06-21 2018-05-31 Иммуноджен, Инк. Новые производные майтанзиноида с пептидным линкером и их конъюгаты

Also Published As

Publication number Publication date
JP2014520156A (ja) 2014-08-21
SG10201605041VA (en) 2016-08-30
EA029797B1 (ru) 2018-05-31
EP2723389A2 (en) 2014-04-30
CA2836927A1 (en) 2012-12-27
JP6598821B2 (ja) 2019-10-30
US10494423B2 (en) 2019-12-03
NZ618262A (en) 2016-03-31
JP6209159B2 (ja) 2017-10-04
JP2017197560A (ja) 2017-11-02
AU2012272930A1 (en) 2013-04-18
WO2012177837A2 (en) 2012-12-27
IL230043A (en) 2017-11-30
CN103648532A (zh) 2014-03-19
IL255475A (en) 2018-02-28
EA201792652A3 (ru) 2018-09-28
EA201792652A2 (ru) 2018-05-31
US20130029900A1 (en) 2013-01-31
US9289512B2 (en) 2016-03-22
EA201490095A1 (ru) 2014-05-30
BR112013032928A2 (pt) 2017-01-24
KR20140037208A (ko) 2014-03-26
ZA201308703B (en) 2016-03-30
US20160263238A1 (en) 2016-09-15
WO2012177837A3 (en) 2013-07-11
MX350954B (es) 2017-09-26
MX2013015422A (es) 2014-09-22
AU2012272930B2 (en) 2015-06-11

Similar Documents

Publication Publication Date Title
SG195172A1 (en) Novel maytansinoid derivatives with peptide linker and conjugates thereof
WO2012145112A3 (en) Novel maytansinoid derivatives with sulfoxide linker
MY183977A (en) Cytotoxic benzodiazepine derivatives
PH12017500358A1 (en) Cytotoxic benzodiazepine derivatives
TW201613930A (en) Cytotoxic benzodiazepine derivatives
SG10201901825YA (en) Conjugates comprising cell-binding agents and cytotoxic agents
PH12014501229A1 (en) Antibody-drug conjugates and related compounds, compositions, and methods
MX366955B (es) Crlx101 para usarse en el tratamiento de cáncer.
MX2013005046A (es) Agentes citotoxicos que comprenden nuevos derivados de ansamitocina.
PH12015500667A1 (en) Antibody-drug conjugate
NZ724892A (en) Self-stabilizing linker conjugates
PH12014501924A1 (en) Xten conjugate compositions and methods of making same
MX368966B (es) Conjugados de proteina-polimero-farmaco.
NZ610239A (en) Cross-linkers and their uses
PT2313111E (pt) Formulações de agonista de receptor do tipo toll e seus usos
NZ599045A (en) New maytansinoids and the use of said maytansinoids to prepare conjugates with an antibody
MX2014007125A (es) Uso de n-hidroxisuccinimida para mejorar la estabilidad de conjugados.
SG195192A1 (en) Non-peptidyl polymer-insulin multimer and method for producing the same
PH12015501980A1 (en) Pyrroloquinolinyl-pyrrolidine-2,5-dione formulations and methods for preparing and using same
UA113162C2 (xx) Цитотоксичні похідні бензодіазепіну
BR112013023599A2 (pt) método para preparar um conjugado de carboidrato-epítopo de célula-t, conjugado de carboidrato-epítopo de célula-t, e, uso de um conjugado de carboidrato-epítopo de célula-t
EA201992044A3 (ru) Цитотоксические бензодиазепиновые производные
MY140324A (en) Maleimide derivatives, pharmaceutical compositions and methods for treatment of cancer
MY148385A (en) Maleimide derivatives, pharmaceutical compositions and methods for treatment of cancer